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Synthesis and first evaluation of new 18 F‐labelled sulfonylureas for the determination of the beta‐cell status in vivo
Author(s) -
Schirrmacher R.,
Shiue G.,
Shiue S. J.,
Alavi A.,
Feilen P. J.,
Schneider S.,
Beyer J.,
Rösch F.
Publication year - 2001
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.25804401148
Subject(s) - chemistry , tolbutamide , formamide , glibenclamide , sulfonylurea , in vivo , urea , fluoride , beta (programming language) , medicinal chemistry , derivative (finance) , stereochemistry , insulin , organic chemistry , endocrinology , inorganic chemistry , medicine , microbiology and biotechnology , computer science , programming language , biology , diabetes mellitus , financial economics , economics
The syntheses and first in vitro evaluations for two fluoride bearing sulfonylurea derivatives are reported. Firstly, the tolbutamide derivative 1‐[4‐(2‐[ 18 F]fluoroethoxy)benzenesulfonyl]‐3‐butyl urea (2‐[ 18 F]fluoroethyl‐tolbutamide) could be labeled efficiently with [ 18 F]fluoride. Subsequently, the glibenclamid derivative N‐(2‐(4‐(N‐((cyclohexylamino)carbonyl)sulfonylamino)phenyl)ethyl) 2‐(5‐chloro‐2‐[ 18 F]fluorethoxy)phenyl) formamide (2‐[ 18 F]fluoroethyl‐glibenclamide) was labeled with [ 18 F]fluoride in high yields. Its ability to induce insuline secretion from rat beta‐cells in relation to the original glibenclamide was determined.